Urotensin II (UII) is a cyclic neuropeptide that was first isolated from the urophysis of teleost fish on the basis of its ability to contract the hindgut. Subsequently, UII was characterized in tetrapods including humans. Phylogenetic studies and synteny analysis indicate that UII and its paralogous peptide urotensin II-related peptide (URP) belong to the somatostatin/cortistatin superfamily. In mammals, the UII and URP genes are primarily expressed in cholinergic neurons of the brainstem and spinal cord. UII and URP mRNAs are also present in various organs notably in the cardiovascular, renal, and endocrine systems. UII and URP activate a common G protein-coupled receptor, called UT, that exhibits relatively high sequence identity with somatostatin, opioid, and galanin receptors. The UT gene is widely expressed in the central nervous system (CNS) and in peripheral tissues including the retina, heart, vascular bed, lung, kidney, adrenal medulla, and skeletal muscle. Structure-activity relationship studies and NMR conformational analysis have led to the rational design of a number of peptidic and nonpeptidic UT agonists and antagonists. Consistent with the wide distribution of UT, UII has now been shown to exert a large array of biologic activities, in particular in the CNS, the cardiovascular system, and the kidney. Here, we review the current knowledge concerning the pleiotropic actions of UII and discusses the possible use of antagonists for future therapeutic applications.

中文翻译：

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国际基础和临床药理学联盟。XCII。尿加压素II，与尿加压素II相关的肽及其受体：从结构到功能。

Urotensin II（UII）是一种环状神经肽，首先基于硬骨鱼的后肠收缩能力从硬骨鱼的尿道中分离出来。随后，UII在包括人类在内的四足动物中被表征。系统发育研究和协同分析表明，UII及其旁系同源肽urotensin II相关肽（URP）属于生长抑素/皮质抑素超家族。在哺乳动物中，UII和URP基因主要在脑干和脊髓的胆碱能神经元中表达。UII和URP mRNA也存在于各种器官中，特别是在心血管，肾脏和内分泌系统中。UII和URP激活共同的G蛋白偶联受体，称为UT，该受体与生长抑素，阿片类和甘丙肽受体具有相对较高的序列同一性。UT基因在中枢神经系统（CNS）和周围组织（包括视网膜，心脏，血管床，肺，肾，肾上腺髓质和骨骼肌）中广泛表达。结构活性关系研究和NMR构象分析已导致合理设计了许多肽类和非肽类UT激动剂和拮抗剂。与UT的广泛分布相一致，UII已被证明具有多种生物活性，特别是在CNS，心血管系统和肾脏中。在这里，我们回顾了有关UII的多效作用的当前知识，并讨论了拮抗剂在未来治疗应用中的可能用途。结构活性关系研究和NMR构象分析已导致合理设计了许多肽类和非肽类UT激动剂和拮抗剂。与UT的广泛分布相一致，UII已被证明具有多种生物活性，特别是在CNS，心血管系统和肾脏中。在这里，我们回顾了有关UII的多效作用的当前知识，并讨论了拮抗剂在未来治疗应用中的可能用途。结构活性关系研究和NMR构象分析已导致合理设计了许多肽类和非肽类UT激动剂和拮抗剂。与UT的广泛分布相一致，UII已被证明具有多种生物活性，特别是在CNS，心血管系统和肾脏中。在这里，我们回顾了有关UII的多效作用的当前知识，并讨论了拮抗剂在未来治疗应用中的可能用途。